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Technical Data
| Formula | C24H32N6O3 |
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| Molecular Weight | 452.55 | CAS No. | 1124329-14-1 | |
| Solubility (25°C)* | In vitro | Ethanol | 11 mg/mL (24.3 mM) | |
| DMSO | 8 mg/mL (17.67 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | AZ3146 is a selective Mps1 inhibitor with IC50 of ~35 nM, contributes to recruitment of CENP-E (kinesin-related motor protein), less potent to FAK, JNK1, JNK2, and Kit. | ||
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| In vitro | AZ3146 also inhibits FAK, JNK1, JNK2 and Kit. AZ3146 significantly inhibits phosphorylation of Mps1 in cells. Mitotic-specific phospho forms of aurora B and BubR1 are not affected by AZ3146. AZ3146 does not inhibit Cdk1 or aurora B in mitotic cells. HeLa cells treated with nocodazole and 2 μM AZ3146 only delay mitosis briefly and then rereplicate their genomes, indicating that AZ3146 overrides the SAC. AZ3146 also inhibits an already established SAC signal, as after release from a nocodazole block, AZ3146 dramatically accelerates mitotic exit.During an otherwise unperturbed mitosis, AZ3146 reduces the time to complete mitosis from 90 minutes in controls to 32 minutes. Strikingly, ~90% of AZ3146-treated HeLa cells undergo abnormal mitoses, although ~50% enter anaphase without aligning all of their chromosomes, and ~30% exit mitosis without undergoing obvious chromosome segregation. AZ3146 has a dramatic effect on kinetochore localization of Mad2, reducing its levels to ~15%, but its effect on Mad1 is less pronounced, with levels remaining at ~60%. When Mps1 is inhibited by AZ3146 before mitotic entry, subsequent recruitment of Mad1 and Mad2 to kinetochores is abolished. However, if Mps1 is inhibited by AZ3146 after mitotic entry, the Mad1–C-Mad2 core complex remains kinetochore bound, but O-Mad2 is not recruited to the core. [1] |
Protocol (from reference)
Customer Product Validation
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Data from [Oncogenesis, 2014, 21, 3:e100]
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Data from [Data independently produced by J Biol Chem, 2013, 288(49), 35149-58]
Selleck's AZ 3146 has been cited by 27 publications
| Design and Validation of Flim-timer for Measuring Protein Turnover in Cells Using Fluorescence Lifetime [ Research Square, 2024, 10.21203/rs.3.rs-2161438/v1] | PubMed: none |
| Molecular landscape and functional characterization of centrosome amplification in ovarian cancer [ Nat Commun, 2023, 14(1):6505] | PubMed: 37845213 |
| Selective utilization of non-homologous end-joining and homologous recombination for DNA repair during meiotic maturation in mouse oocytes [ Cell Prolif, 2023, 56(4):e13384] | PubMed: 36564861 |
| CWH43 Is a Novel Tumor Suppressor Gene with Negative Regulation of TTK in Colorectal Cancer [ Int J Mol Sci, 2023, 24(20)15262] | PubMed: 37894942 |
| CWH43 Is a Novel Tumor Suppressor Gene with Negative Regulation of TTK in Colorectal Cancer [ Int J Mol Sci, 2023, 24(20)15262] | PubMed: 37894942 |
| Remarkable Synergy When Combining EZH2 Inhibitors with YM155 Is H3K27me3-Independent [ Cancers (Basel), 2022, 15(1)208] | PubMed: 36612203 |
| Mitotic phosphorylation of tumor suppressor DAB2IP maintains spindle assembly checkpoint and chromosomal stability through activating PLK1-Mps1 signal pathway and stabilizing mitotic checkpoint complex [ Oncogene, 2021, 10.1038/s41388-021-02106-8] | PubMed: 34775484 |
| Unrestrained ESCRT-III drives micronuclear catastrophe and chromosome fragmentation [ Nat Cell Biol, 2020, 22(7):856-867] | PubMed: 32601372 |
| A kinase-independent function for AURORA-A in replisome assembly during DNA replication initiation [ Nucleic Acids Res, 2020, gkaa570] | PubMed: 32652013 |
| Single-Chromosomal Gains Can Function as Metastasis Suppressors and Promoters in Colon Cancer. [ Dev Cell, 2020, 52(4):413-428] | PubMed: 32097652 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.